Cholinergic Agents Flashcards Preview

Med Chem > Cholinergic Agents > Flashcards

Flashcards in Cholinergic Agents Deck (23):
1

Acetylcholine (Ach)

Neurotransmitter that plays a critical role in muscle contraction and restriction

2

Nicotinic receptors

Bound by nicotine
When Ach binds, channels are opened, and the nerve is depolarized, leading to muscular contraction or continuation of the nerve impulse

3

N1 receptors

Located at neuromuscular junction

4

N2 receptors

Located in autonomic nerves

5

Muscarinic receptors

Bound by muscarine or Ach
Regulate organs innervated by the autonomic nervous system to maintain homeostasis
7-domain G-protein coupled receptors

6

M1 receptors

Wide variety of functions, including REM sleep, emotional regulation, and gastric secretion

7

M2 receptors

Also called cardiac muscarinic receptors
Function in respiration

8

M3 receptors

Stimulate glandular secretions and contract smooth muscle

9

M4 receptors

Act on G proteins to inhibit cAMP (secondary messenger)

10

Cholinergic receptors can be selective based on...

Stereochemistry

11

5-atom rule

Muscarinic activity is maximized by a chain of 5 carbon atoms following a quaternary ammonium group

12

Cholinergic agents SAR

Alpha and beta substitutions (relative to N) decrease cholinergic activity
Alpha: greater muscarinic change
Beta: greater nicotinic change

13

Acetylcholinesterase

Catalyzes the hydrolysis of Ach to choline and acetic acid

14

Butyrylcholinesterase

Biological function isn't clear (has catalytic properties similar to acetylcholinesterase)

15

Carbamates

Semi-reversible inhibitors of acetylcholinesterase

16

Organophosphates

Irreversible inhbitors of acetylcholinesterase

17

Cholinergic blocking agents

Inhibit the effect of Ach on cholinergic receptors
SAR: structurally similar to Ach but with additional substituents (hydroxyl group, cyclic substitution)

18

Parasympathetic postganglionic blocking agents

3 therapeutic effects: dilation of pupils, slowing down of digestion, decrease in secretions

19

Synthetic cholinergic blocking agents

Aminoalcohol esters (bind tightly to M1 and M3 receptors)
Aminoalcohol ethers
Aminoalcohols
Aminoamides

20

Ganglionic blocking agents

Nondepolarizing competitive or nondepolarizing noncompetitive (treat hypertension by blocking sympathetic pathways)

21

Neuromuscular blocking agents

Block transmission of Ach at the motor end plate
Relax skeletal muscle during surgical anesthesia

22

Nondepolarizing blocking agents

Compete with Ach at the end plate receptors

23

Depolarizing blocking agents

Desensitize end plate through repeated bombardment of Ach